Condom

ABSTRACT

A condom has a vasodilator active compound applied to its external surface, preferably disposed towards the open end of the condom whereby, in use during intercourse, the compound makes contact with the vaginal meatus or proximal region of the vagina, such that the vasodilator is absorbed though the lining of the vagina to stimulate and increase the flow of blood in the labia and through the clitoris to promote engorgement thereof to alleviate symptoms associated with female inorgasmia

This invention relates to condoms and is particularly intended toprovide a condom for provision of sexual stimulation to the femalepartner of the user, in order to alleviate female sexual dysfunction, toenhance sexual pleasure and to improve condom safety through loweringcondom failure due to rupture, by increasing vaginal secretion andlubrication.

It is recognised that female sexual dysfunction is a complex conditionwhich, due to its various causes, cannot readily be treated by use of aparticular drug or device. Nevertheless, an increase in vaginal bloodflow and clitoral engorgement is known to be associated with increasedvaginal secretions, a decrease in dyspareunia and increases in clitoralsensation, orgasmic response and sexual desire. It is an object of thepresent invention, therefore, to provide a means of stimulating thefemale genitalia during intercourse to increase vaginal blood flow.

In one aspect, the invention provides a condom having applied to itsexternal surface a vasodilator active compound.

The vasodilator active compound is preferably disposed and retained in alocalised region towards the open end of the condom whereby, in useduring intercourse, the compound makes contact with the vaginal meatusor proximal region of the vagina, such that the vasodilator is absorbedthrough the lining of the vagina to stimulate and increase the flow ofblood in the labia and through the clitoris to promote engorgementthereof which, itself,, will lead to further or enhanced stimulation andresult in increased vaginal secretions. Symptoms associated with femaleinorgasmia will thus be alleviated.

By use of the invention, a further advantage is that increased vaginalsecretions result in increased lubrication between the wall of thevagina and the condom resulting in a lower rate of condom failure due torupture.

In condoms according to the present invention, the active compound maybe contained or impregnated in or coated on the external surface of thecondom. The vasodilator may be applied as a composition which includes acarrier material with which the vasodilator compound is miscible butwhich will release the vasodilator active compound when in contact withbody tissue. Where the condom is coated with a lubricant, thevasodilator active compound may be dispersed or dissolved in thelubricant but preferably is disposed on the condom surface in a form orwithin a composition which is immiscible with the lubricant, whereby thecompound is localised substantially at the zone of application to thecondom surface. The active compound on such condoms, when they are intheir rolled-up state for packaging purposes, thus tends to resisttranslocation from the external surface to adjacent portions of theinternal surface, whereby the active compound is retained predominantlyon the external surface and within the original zone of application.Preferably, the lubricant is buffered to an acidic pH, for examplebetween 3 to 5, to prevent hydrolysis of the vasodilator activecompound.

Condoms according to the present invention may include a textured orundulating region to the external surface, to provide enhanced physicalstimulation to the female genitalia during intercourse to increasesexual sensation. The textured or undulating region may be locatedtowards the open end of the condom so that the proximal parts of thevagina and the clitoris are preferentially stimulated by contact withthe texturing or undulations. The textured or undulating regionpreferably incorporates or includes the vasodilator active compound. Thetexturing or undulations may comprise ribs or an array of individualprotrusions or may comprise merely a roughened surface region, formedeither by imparting a pattern to the surface of the condom or byapplication to the surface thereof of a particulate material or amaterial having a high coefficient of surface friction, such as a highlyplasticised elastomer. The textured surface may be formed bymanufacturing the condom on a mandrel or mould having an appropriatepattern of ribs, dots or other texturing etched into or embossed on itssurface or by applying to the condom a material which results in atextured surface, for example by extruding a thin stream of the materialfrom a nozzle so as to form a series of rings around the condom or byspraying the material in such a way that the surface becomes textured. Asuitably textured extruded section can be applied direct to the condomat the time of its manufacture or subsequently, either by direct bondingor by the use of a pressure-sensitive, hot-melt or other suitable typeof adhesive. Alternatively, a coating of a material can be applied forexample by spraying, the coating then having a texturing applied to itby contact with a suitably patterned die so as to mould the surface inthe desired textured shape.

The textured surface may be formed from one or more layers of materialincluding the material from which the condom itself is formed. Thematerial of at least one such layer should be miscible with thevasodilator and should allow the vasodilator to be absorbed by skin ortissue when brought in contact with the condom. Preferably, the materialfrom which the condom is formed, either natural rubber latex or asynthetic rubber-like material, and any lubricant used therein, isimmiscible with the vasodilator or the vasodilator-containingcomposition, whereby the vasodilator is restrained from migrating toother parts of the condom other than the zone of application. Thematerial from which the vasodilator-containing layer is formed willdepend on the nature of the vasodilator active compound but, for activecompounds such as organic nitrates, for example glyceryl trinitrate,suitable materials would include polar elastomers applied to the condomfrom solution, in the form of an aqueous dispersion of latex or by a hotmelt or reactive process. Alternatively, the vasodilator-containinglayer can be pre-formed and bonded subsequently to the condom using asuitable adhesive system as necessary.

The vasodilator active compound may comprise any known erectogeniccompound which, on absorption through the skin or mucosa, locallyenhances blood flow. Such compounds may include nitrates, long and shortacting alpha-adrenoceptor blockers, ergot alkaloids, anti-hypertensivesand the prostaglandins. Phosphodiesterase inhibitors, particularly typeIII and IV and most particularly type V can also be used, either aloneor in combination with other vasodilators. Such compounds can be usedalone or in combination and, optionally, together with skin penetrationenhancers such as azone, dimethylsulfoxide, dimethyl formamide,N,N-dimethylacetamide, declymethylsulfoxide, polyethylene glycolmonolaurate, glycerol monolaurate, lecithin and 1-substitutedazacyclopheptan-2-one.

Useful nitrates and similarly acting compounds include nitro-glycerine,isosorbide dinitrate, erythrityl tetranitrate, amyl nitrate, sodiumnitroprusside, molsidomine, linsidomine chlorydrate (“SIN-1”),S-nitroso-N-acetyl-d,1-penicillaamine (“SNAP”), S-nitroso-N-cysteine,S-nitroso-N-glutathione (“SNO-GLU”) and diazenium diolates (“NONOates”).A particularly useful nitrate is nitro-glycerine.

Natural prostaglandins that can be used include PGE₀, PGE₁, PGA₁, PGB₁,PGF₁alpha, 19-hydroxy-PGA₁, 19-hydroxy-PGB₁, PGE2, PGA₂, PGB₂,19-hydroxy-PGA₂, 19-hydroxy-PGB₂, PGE₃, PGF₃alpha. Semi synthetic andsynthetic prostaglandins such as carboprost tromethamine, dinoprosttromethamine, dinoprostone, lipoprost, gemeprost, metenoprost,sulprostone and tiaprost can also be used. A particularly usefulprostaglandin is prostaglandin E₁ (PGE₁) or its synthetic version,alprostadil. Esters of the prostaglandins, such as the methyl and ethylesters, can also be used.

Suitable alpha-adrenoceptor blockers include phenoxybenzamine,dibenamine, doxazosin, terazosin, phentolamine, tolazoline, prazosin,trimazosin, alfuzosin, tamsulosin and indoramin.

Ergot alkaloids include ergotamine and ergotamine analogs, e.g.,acetergamine, brazergoline, bromerguride, cianergoline, delorgotrile,disulergine, ergonovine maleate, ergotamine tartrate, etisulergine,lergotrile, lysergide, mesulergine, metergoline, metergotamine,nicergoline, pergolide, propisergide, proterguride and terguride. Aparticularly effective alkaloid is yohimbine hydrochloride.

Non-specific phosphodiesterase inhibitors that can be incorporated intothe condom include theophylline, IBMX, pentoxifylline and papaverine,and direct vasodilators such as hydralazine. Papaverine is particularlyuseful either alone or in combination with phentolamine.

Examples of type III phosphodiesterase inhibitors that may be usedinclude bipyridines such as milrinone and amirinone, imidazolones suchas piroximone and enoximone, dihydropyridazinones such as imazodan,5-methyl-imazodan, indolidan and ICI1118233, quinolinone compounds suchas cilostamide, cilostazol and vesnarinone, and other molecules such asbemoradan, anergrelide, siguazodan, trequinsin, pimobendan, SKF-94120,SKF-95654, lixazinone and isomazole.

Examples of suitable type IV phosphodiesterase inhibitors includerolipram and rolipram derivatives such as RO20-1724, nitraquazone andnitraquazone derivatives such as CP-77059 and RS-25344-00, xanthinederivatives such as denbufylline and ICI63197, and other compounds suchas EMD54622, LAS-31025 and etazolate.

Examples of type V phospodiesterase inhibitors include zaprinast,MY5445, dipyridamole, vardenafil, and sildenafil. Other suitable type Vphosphodiesterase inhibitors are disclosed in PCT Publication Nos. WO94/28902 and WO 96/16644. A particularly useful type V phosphodiesteraseinhibitor is sildenafil. Still other type V phosphodiesterase inhibitorsuseful in conjunction with the present invention include: IC-351 (ICOS);4-bromo-5-(pyridylmethylamino)-6-[3-(4-chlorophenyl)propoxy]-3(2H)pyridazinone;1-[4-[(1,3-benzodioxol-5-ylmethyl)amino]-6-chloro-2-quinazolinyl]-4-piperidine-carboxylicacid, monosodium salt;(+)-cis-5,6a,7,9,9a-hexahydro-2-[4-(trifluoromethyl)-phenylmethyl-5-methyl-cyclopent-4,5]imidazo[2,1-b]purin-4(3H)one,furazlocillin;cis-2-hexyl-5-methyl-3,4,5,6a,7,8,9,9a-octahydrocyclopent[4,5]imidazo[2,1-b]purin-4-one;3-acetyl-1-(2-chlorobenzyl)-2-propylindole-6-carboxylate;4-bromo-5-(3-pyridylmethylamino)-6-(3-(4-chlorophenyl)propoxy)-3-(2H)pyridazinone;1-methyl-5-(5-morpholinoacetyl-2-n-propoxyphenyl)-3-n-propyl-1,6,-dihydro-7H-pyrazolo(4,3-d)pyrimidin-7-one;1-[4-[1,3-benzodioxol-5-ylmethyl)amino]-6-chloro-2-quinazolinyl]4-piperidinecarboxylicacid, monosodium salt; Pharmaprojects No. 4516 (Glaxo Wellcome);Pharmaprojects No. 5051 (Bayer); Pharmaprojects No. 5064 (Kyowa Hakko;see WO 96/26940); Pharmaprojects No. 5069 (Scherin Plough); GF-196960(Glaxo Wellcome); and Sch-51866.

Other compounds that can be used include nimodipine, pinacidil,cyclandelate, isoxsuprine, chloromazine, haloperidol, Rec15/2739 andtrazodone, as well as anti-hyertensive agents including diazoxide,hydralazine and minoxidil.

The active compound or compounds optionally together with skinpenetration enhancers may be applied direct to the appropriate region ofthe condom or as a composition dispersed or dissolved in a suitablecarrier media, for example a gel carrier comprising a liquid medium anda thickening agent. According to another aspect of the invention,therefore, a composition for application to the external surface of acondom after unrolling on an erect penis comprises a vasodilator activecompound and a carrier material.

In yet another embodiment, the invention provides a method of treatingfemale sexual dysfunction, the method comprising the use during sexualintercourse of a condom having applied to the external surface avasodilator active compound.

A condom according to the invention may also have a vasodilator activecompound applied to the interior surface, in order to assist inmaintaining an erection of the penis and, thus, providing for additionalcondom safety in prevention of premature and involuntary unsheathing ofthe condom from an otherwise partially-erect or flaccid penis. Acompound applied to the interior surface may be localised at or towardsthe head end and may be the same or a different active compound to thatapplied to the external surface.

Embodiments of the invention will now be described by way of exampleonly.

EXAMPLE 1

A condom having a textured portion towards the open end was made bydipping a former into compounded natural rubber latex, the former havinga series of groves etched into its surface so as to form a series ofribs near the open end of the condom. After the condom was removed fromthe former it was mounted on a mandrel and a thin coating of aplasticised thermoplastic elastomer (a tri-block copolymer of styreneand butadiene) dissolved in a suitable solvent containing glyceroltrinitrate absorbed onto lactose was applied by roller to the ribbedportion of the condom. The solvent was evaporated to leave the coatingon the textured portion. The condoms were then rolled off the mandreland lubricated and packed as normal. A water-based lubricant, which isimmiscible with glycerol trinitrate, was selected. The presence of thelactose enhanced the texture of the ribs and acted as a source ofglycerol trinitrate.

EXAMPLE 2

A 10 mm wide strip of a plasticised thermoplastic elastomer containingglycerol trinitrate dissolved in monopropylene glycol was extruded ontorelease paper using a die to form a profile having a number of raisedribs. The extruded strip, still on the release paper, was cut into anumber of strips, the length of each strip being the circumference ofthe condom. Standard, parallel sided, non-ribbed condoms were mountedonto suitable mandrels and the strips were wrapped around the condomsnear to the open end. The strips were then made to adhere to the condomby applying a heated roller and the release paper was removed. Thecondoms were then rolled, lubricated and packed as normal.

EXAMPLE 3

A standard, un-ribbed condom was mounted on a mandrel and a thin film ofa plasticised thermoplastic elastomer dissolved in a suitable solventwas sprayed onto the condom in a narrow band close to its open end. Theelastomer contained glycerol trinitrate dissolved in monopropyleneglycol. The solvent was removed by evaporation and the mandrel wasbrought into contact with a hot embossed roller so that the rollerpressed onto the band. The mandrel was rotated so as to leave anembossed pattern in the band. The condom was removed from the mandreland then lubricated and packed.

1. A condom having applied to its external surface a vasodilator activecompound and being coated with a lubricant, characterised in that thevasodilator active compound is disposed on the external condom surfacein a form or within a composition which is immiscible with thelubricant.
 2. A condom according to claim 1, in which the vasodilatoractive compound is disposed towards the open end of the condom.
 3. Acondom according to claim 1 or claim 2, in which the active compound isapplied as a composition which includes a carrier material with whichthe vasodilator compound is miscible but which will release thevasodilator active compound when in contact with body tissue.
 4. Acondom according to any preceding claim, in which the lubricant isbuffered to a pH between 3 and
 5. 5. A condom according to any precedingclaim, in which the condom includes a textured or undulating region tothe external surface.
 6. A condom according to claim 5, in which thetextured or undulating region extends at least towards the open end ofthe condom and incorporates or includes the vasodilator active compound.7. A condom according to claim 6, in which the textured or undulatingregion is formed from one or more layers of material including thematerial from which the condom itself is formed, the material of atleast one such layer being miscible with the vasodilator and allowingthe vasodilator to be absorbed by skin or tissue when brought in contactwith the condom.
 8. A condom according to any preceding claim, in whichthe vasodilator active compound is selected from nitrates, long andshort acting alpha-adrenoceptor blockers, ergot alkaloids,anti-hypertensives, the prostaglandins and phosphodiesterase inhibitorsoptionally in combination with a skin penetration enhancer.
 9. A condomaccording to claim 8, in which the vasodilator active compound comprisesan organic nitrate applied as a layer or coating in a polar elastomer insolution, in the form of an aqueous dispersion of latex or by a hot meltor reactive process.
 10. A condom according to any preceding claim, inwhich the active compound optionally together with a skin penetrationenhancer is applied to the condom as a composition dispersed ordissolved in a gel carrier comprising a liquid medium and a thickeningagent.